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Related Concept Videos

Proteomics01:33

Proteomics

A proteome is the entire set of proteins that a cell type produces. We can study proteomes using the knowledge of genomes because genes code for mRNAs, and the mRNAs encode proteins. Although mRNA analysis is a step in the right direction, not all mRNAs are translated into proteins.
Proteomics is the study of proteomes' function. It involves the large-scale systematic study of the proteome to denote the protein complement expressed by a genome. Scientist Mark Wilkins coined the term proteomics...

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Mapping Dysfunctional Protein-Protein Interactions in Disease
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Chemical kinomics: a powerful strategy for target deconvolution.

Do-Hee Kim1, Taebo Sim

  • 1Life/Health Division, Korea Institute of Science and Technology, Seoul 130-650, Korea.

BMB Reports
|November 30, 2010
PubMed
Summary

Chemical kinomics utilizes small molecules to understand cellular signaling and discover kinase drugs. This approach identifies new drug targets and leads, as demonstrated by a novel Bcr-Abl inhibitor.

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Characterization at the Molecular Level using Robust Biochemical Approaches of a New Kinase Protein
11:23

Characterization at the Molecular Level using Robust Biochemical Approaches of a New Kinase Protein

Published on: June 30, 2019

Area of Science:

  • Biochemistry
  • Chemical Genomics
  • Pharmacology

Background:

  • Kinomics offers a promising avenue for kinome deciphering.
  • Chemical kinomics, a sub-discipline of chemical genomics, leverages small molecules to modulate kinase functions.
  • This approach is crucial for understanding complex phosphorylation-based cellular signaling networks.

Purpose of the Study:

  • To review contemporary chemical kinomics technologies.
  • To highlight the role of chemical kinomics in kinase drug discovery.
  • To showcase a successful application of chemical kinomics in identifying a novel kinase inhibitor.

Main Methods:

  • Activity-based protein profiling
  • T7 kinase-tagged phages
  • Kinobeads
  • Three-hybrid systems
  • Fluorescent-tagged kinase binding assays
  • Chemical genomic profiling

Main Results:

  • Chemical kinomics enables the identification of new molecular targets for small molecule kinase modulators.
  • It facilitates the discovery of novel functions for known kinases.
  • Novel chemical entities have been identified as hit/lead compounds.
  • A novel allosteric Bcr-Abl kinase inhibitor (GNF-2/GNF-5) exemplifies successful chemical kinomics application.

Conclusions:

  • Chemical kinomics is a powerful approach for deciphering kinase biology and signaling pathways.
  • It plays a pivotal role in advancing kinase drug discovery.
  • The discussed technologies and the GNF-2/GNF-5 inhibitor demonstrate the potential of chemical kinomics.